Design and development of donepezil hydrochloride loaded nanostructured lipid carriers for efficient management of Alzheimer's disease.

IF 2.4 4区 医学 Q3 CHEMISTRY, MEDICINAL
Avinash R Tekade, Mayuri R Suryavanshi, Ashutosh B Shewale, Vilas S Patil
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引用次数: 0

Abstract

Objective: The primary objective of this study was to develop nanostructured lipid carriers of donepezil hydrochloride (DNZ HCl) for effective management of Alzheimer's disease (AD).

Significance: Intranasal administration of DNZ NLC containing Nigella sativa (NS) oil as a liquid lipid may significantly improve nasal penetration and deliver the drug directly to the brain avoiding blood brain barrier (BBB).

Method: High pressure homogenization was used to prepare nanostructured lipid carriers (NLCs), followed by ultrasonication. Glyceryl monostearate (GMS), Tween 80, and Poloxamer 407 were used as solid lipid, surfactant and co-surfactant respectively, whereas, Nigella sativa oil was used as a liquid lipid.

Result: The particle size, polydispersity index and zeta potential were found to be 107.4 ± 2.64 nm, 0.25 ± 0.04 and -41.7 mV. The entrapment efficiency and drug content were found to be 70.20% and 89.05% respectively. After intranasal administration of Donepezil hydrochloride (DNZ HCl) loaded NLC's, the maximum concentrations (Cmax) of 4.597 µg/mL in brain and 2.2583 µg/mL in blood was achieved after 1 h (Tmax).

Conclusion: The formulated DNZ HCl loaded NLCs significantly improved nasal penetration and enhanced drug distribution in brain resulting in a potentially effective intranasal drug delivery system for the effective management of Alzheimer's disease.

盐酸多奈哌齐负载纳米结构脂质载体的设计和开发,用于有效治疗阿尔茨海默病。
目的:本研究的主要目的是开发盐酸多奈哌齐(DNZ-HCl)的纳米结构脂质载体,以有效治疗阿尔茨海默病方法:采用高压均质法制备纳米脂质载体(NLCs),然后进行超声处理。单硬脂酸甘油酯(GMS)、吐温80和泊洛沙姆407分别用作固体脂质、表面活性剂和助表面活性剂,而奈杰尔籽油用作液体脂质。结果:样品的粒径、多分散指数和ζ电位为107.4 ± 2.64 nm,0.25 ± 0.04和-41.7 包封率和药物含量分别为70.20%和89.05%。经鼻给药盐酸多奈哌齐(DNZ-HCl)负载NLC后,最大浓度(Cmax)为4.597 µg/mL脑内和2.2583 1 h(Tmax)。结论:配制的DNZ-HCl负载NLCs显著改善了鼻腔渗透性,增强了药物在大脑中的分布,从而形成了一种潜在有效的鼻内药物递送系统,用于有效治疗阿尔茨海默病。
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来源期刊
CiteScore
6.80
自引率
0.00%
发文量
82
审稿时长
4.5 months
期刊介绍: The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.
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